Lomitapide
(Synonyms: 洛美他派; AEGR-733; BMS-201038) 目录号 : GC16870
An MTTP inhibitor
Cas No.:182431-12-5
Sample solution is provided at 25 µL, 10mM.
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Lomitapide (AEGR-733, BMS-201038) is an oral inhibitor of microsomal triglyceride transfer protein [1].
Microsomal triglyceride transfer protein (MTP) plays an important role in lipoprotein assembly. The mutation of MTP can cause abetalipoproteinemia.
Lomitapide is a MTP inhibitor and used for the treatment of homozygous familial hypercholesterolemia. In patients with familial hypercholesterolemia, lomitapide reduced low-density lipoprotein cholesterol (LDL-C) by more than 50% both as monotherapy and in combination with prescribed lipid-lowering therapies [1]. Lomitapide bound to and inhibited MTP within the lumen of the endoplasmic reticulum and inhibited the synthesis of VLDL and chylomicrons, resulting in the reduction of circulating LDL-C concentrations. In human, lomitapide (50 mg) reduced apo B, LDL-C and total cholesterol concentrations in a dose dependent way. However, lomitapide caused significant gastrointestinal (GI) disturbances at the concentration of 100 mg [2].
References:
[1]. Rizzo M. Lomitapide, a microsomal triglyceride transfer protein inhibitor for the treatment of hypercholesterolemia. IDrugs, 2010, 13(2): 103-111.
[2]. Davis KA, Miyares MA. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm, 2014, 71(12): 1001-1008.
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Animal experiment: |
Rats: BMS-201038 is formulated in 0.1% hydroxyl ethyl cellulose and 0.5% Tween 80 in deionized water. Rats in the control group are administered vehicle (2 mL/kg) p.o. Fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by 250 mg/kg, i.v., Triton WR1339. Blood samples are obtained from rats up to 240 min after Triton WR1339 injection to estimate serum triglyceride concentrations. For evaluation of post-prandial lipaemia, fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by a corn oil bolus (6 mL/kg) by oral gavage. Blood samples are again collected up to 1440 min after corn oil administration for the estimation of serum triglyceride concentrations[3]. |
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References: [1]. Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. |
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| Cas No. | 182431-12-5 | SDF | |
| 别名 | 洛美他派; AEGR-733; BMS-201038 | ||
| 化学名 | N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide | ||
| Canonical SMILES | C1CN(CCC1NC(=O)C2=CC=CC=C2C3=CC=C(C=C3)C(F)(F)F)CCCCC4(C5=CC=CC=C5C6=CC=CC=C64)C(=O)NCC(F)(F)F | ||
| 分子式 | C39H37F6N3O2 | 分子量 | 692.71 |
| 溶解度 | ≥ 22.4mg/mL in DMSO | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4436 mL | 7.218 mL | 14.4361 mL |
| 5 mM | 0.2887 mL | 1.4436 mL | 2.8872 mL |
| 10 mM | 0.1444 mL | 0.7218 mL | 1.4436 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet